What is Naltrexone (DEPADE) 50mg tablet?

From the Guidelines

Naltrexone (DEPADE) 50mg tablet is an opioid antagonist used to treat alcohol and opioid dependence by blocking opioid receptors in the brain, reducing cravings and the pleasurable effects of these substances. The medication is available as a 50-mg tablet taken daily, with the option of alternative dosing schedules, such as 100 mg on Mondays and Wednesdays, and 150 mg on Fridays 1. It's essential to note that naltrexone should not be used in patients who require opioids for pain control, as it will block the pain-relieving effects of opioid agonists and may precipitate withdrawal symptoms.

When considering the use of naltrexone, it's crucial to prioritize the patient's safety and well-being. Patients should be opioid-free for at least 7-10 days before starting naltrexone, and liver function tests are recommended at baseline and every three to six months due to the potential risk of hepatic injury at supratherapeutic doses 1. Common side effects of naltrexone include nausea, headache, dizziness, anxiety, and fatigue, which typically improve over time.

Some key points to consider when prescribing naltrexone include:

• The medication does not cause dependence and does not produce a high, making it safe for long-term use under medical supervision.
• Naltrexone has been shown to be helpful in maintaining abstinence from opioids in motivated populations, such as healthcare professionals who cannot or do not wish to take continuous opioid agonist therapy 1.
• The use of naltrexone in patients with significant liver disease is not recommended due to the potential risk of hepatotoxicity 1.
• Alternative medications, such as baclofen, may be considered for patients with alcoholic liver disease, as it has been shown to be safe and effective in promoting alcohol abstinence in these patients 1.

In terms of preoperative management, it's recommended to hold naltrexone for 3-4 days before surgery, as concomitant use with opioids can result in reduced opioid efficacy and precipitate opioid withdrawal 1. Overall, naltrexone can be a valuable treatment option for patients with alcohol and opioid dependence, but its use should be carefully considered and monitored to minimize potential risks and maximize benefits.

From the FDA Drug Label

Naltrexone hydrochloride tablets USP 50 mg is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. Naltrexone hydrochloride, an opioid antagonist, is a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone hydrochloride tablets,50 mg is available in film coated tablets, containing 50 mg of naltrexone hydrochloride USP

Naltrexone (DEPADE) 50mg tablet is a film-coated tablet containing 50mg of naltrexone hydrochloride, which is an opioid antagonist used in the treatment of alcohol dependence and for the blockade of opioid effects 2.

• It has no opioid agonist properties and is used as part of a management plan for addictions 2.

From the Research

Naltrexone (DEPADE) 50mg Tablet

• Naltrexone is an opioid receptor antagonist that has been shown to be effective for maintaining abstinence in alcohol-dependent persons 3.
• It is also FDA approved to treat opioid dependence, available as an oral tablet and an extended-release injectable suspension 4.
• The usual dosage of naltrexone hydrochloride is 50 mg orally once daily or 350 mg orally per week in three divided doses 5.
• Naltrexone appears to be a useful adjunct to therapy in opiate addicts who are well motivated and who have strong psychological support systems 5.
• It was first available in the mid-1970s as a 50 mg tablet that blocked opioids for 24-36 h if taken daily, or every 2-3 days at higher doses 6.
• Studies have found that naltrexone, a long-acting opiate antagonist, owing to poor patient compliance, is of limited value in preventing relapse, but compliance can be improved with counseling and ultra-rapid opiate detoxification 7.

Mechanism of Action

• The therapeutic effects of naltrexone are mediated by blockade of central mu opioid receptors 3.
• Naltrexone binds tightly to μ-opioid receptors and blocks the subjective and analgesic effects of opioids 6.
• The site of action is under investigation but evidence supports a role of mu opioid receptors in the central nucleus of the amygdala, nucleus accumbens, and ventral tegmental area in the therapeutic actions of naltrexone for alcohol dependence 3.

Metabolism and Side Effects

• Naltrexone is rapidly and completely absorbed after oral administration but undergoes substantial first-pass extraction and metabolism by the liver 5.
• The major metabolite of naltrexone is 6-beta-naltrexol, which is present in plasma in greater concentrations than the parent drug 5.
• Gastrointestinal irritation and, in some studies, clinically insignificant increases in blood pressure, have been the most common adverse effects 5.
• One of the lesser-known metabolites of naltrexone, noroxymorphone, can cause a positive oxycodone urine drug screen during treatment with oral naltrexone 4.